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BGJ398 (Synonyms: Infigratinib, NVP-BGJ398)

Catalog No.GC10055

An FGFR inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

BGJ398 Chemical Structure

Cas No.: 872511-34-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$40.00
In stock
5mg
$35.00
In stock
10mg
$49.00
In stock
50mg
$101.00
In stock
100mg
$173.00
In stock
200mg
$293.00
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500mg
$606.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment: [1]

Cell lines

AN3CA, MFE296, MFE280, SNGM and HEC1A cells

Preparation method

The solubility of this compound in DMSO is

Reaction Conditions

0.5 μM, 72 hours

Applications

Exposure of AN3CA, MFE296, and MFE280 cells to the inhibitor led to a significant increase in the fraction of cells in G0–G1 arrest and to a significant increase in the fraction of cells undergoing apoptosis, when compared with untreated controls. In contrast, NVP-BGJ398 treatment did not alter the fractions of cells in G0–G1 arrest in the FGFR2 wild-type endometrial cancer cell lines SNGM or HEC1A in vitro. Moreover, NVP-BGJ398 treatment had no effect on apoptosis in the FGFR2 wild-type endometrial cancer cell line HEC1A.

Animal experiment: [1]

Animal models

Nude mice bearing AN3CA, MFE296, SNGM or HEC1A xenografts

Dosage form

Oral administration, 30 or 50 mg/kg, daily

Applications

NVP-BGJ398 significantly delayed the growth of FGFR2-mutated endometrial cancer xenograft tumors. In contrast, NVP-BGJ398 had no in vivo inhibitory effects in the long-term study using the FGFR2 wild-type endometrial cancer cell line SNGM, but surprisingly did show in vivo activity in HEC1A cells by delaying tumor growth in these cells.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Konecny G E, Kolarova T, O'Brien N A, et al. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Molecular cancer therapeutics, 2013, 12(5): 632-642.

Background

NVP-BGJ398 is a potent, selective, and orally bioavailable inhibitor of the FGFR tyrosine kinases. NVP-BGJ398 is a small molecular with the formula of C26H31Cl2N7O3 and Molecular Weight of 560. The fibroblast growth factor receptor 1 (FGFR1), FGFR2, FGFR3, and FGFR4, encompasses the receptors for 18 different FGF ligands. These ligand–receptor combinations regulate a broad spectrum of signaling during development and in normal growth control. BGJ398 inhibits the cell proliferation and induces apoptosis in cancer cells and suppresses tumor growth in xenograft model.

References:
1. Fibroblast Growth Factor Receptors as Novel Therapeutic Targets in SNF5-Deleted Malignant Rhabdoid Tumors. S Wöhrle, A Weiss, M Ito, A Kauffmann, M Murakami. PLOS ONE. 2013
2. Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth. F Harbinski, VJ Craig, S Sanghavi, D Jeffery, L Liu. Cancer Discovery, 2012

Chemical Properties

Cas No. 872511-34-7 SDF
Synonyms Infigratinib, NVP-BGJ398
Chemical Name 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea
Canonical SMILES CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl
Formula C26H31Cl2N7O3 M.Wt 560.48
Solubility ≥ 7mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.7842 mL 8.9209 mL 17.8418 mL
5 mM 0.3568 mL 1.7842 mL 3.5684 mL
10 mM 0.1784 mL 0.8921 mL 1.7842 mL
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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